Speed trap: Cysteamine reacts in DMSO with electrophilic double bonds to afford Michael adducts (see scheme), whereas no trapping reaction takes place in apolar solvents. A simple and quick NMR spectroscopic method to identify Michael acceptors and sort them into reversible and irreversible thiol sinks is validated biologically in a cellular assay sensitive to thiol-trapping agents.
An NMR spectroscopic method to identifiy and classify thiol-trapping agents: revival of Michael acceptors for drug discovery? / C., Avonto; TAGLIALATELA SCAFATI, Orazio; F., Pollastro; A., Minassi; V., Di Marzo; L., De Petrocellis; G., Appendino. - In: ANGEWANDTE CHEMIE. INTERNATIONAL EDITION. - ISSN 1433-7851. - 50:(2011), pp. 467-471. [10.1002/anie.201005959]
An NMR spectroscopic method to identifiy and classify thiol-trapping agents: revival of Michael acceptors for drug discovery?
TAGLIALATELA SCAFATI, ORAZIO;
2011
Abstract
Speed trap: Cysteamine reacts in DMSO with electrophilic double bonds to afford Michael adducts (see scheme), whereas no trapping reaction takes place in apolar solvents. A simple and quick NMR spectroscopic method to identify Michael acceptors and sort them into reversible and irreversible thiol sinks is validated biologically in a cellular assay sensitive to thiol-trapping agents.| File | Dimensione | Formato | |
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